5-methylurapidil [Ligand Id: 489] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL420060
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
  • Alpha-1a adrenergic receptor in Bovine [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
  • Alpha-1a adrenergic receptor in Rabbit [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL The compound was tested for binding affinity against Alpha-1A adrenergic receptor from human clones. B 8.64 pKi 2.3 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity was tested on human Alpha-1A adrenergic receptor B 9.2 pKi 0.63 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
GtoPdb - - 9.2 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
FEBS Lett (1998) 422: 279-83 [PMID:9490024];
J Pharmacol Exp Ther (1996) 278: 136-44 [PMID:8764344];
Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121];
J Pharmacol Exp Ther (1997) 281: 1272-83 [PMID:9190863];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130]
ChEMBL The compound was tested for binding affinity against Alpha-1A adrenergic receptor from bovine clones. B 8.36 pKi 4.4 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor B 9.3 pKi 0.5 nM Ki J Med Chem (1997) 40: 2674-2687 [PMID:9276013]
Alpha-1a adrenergic receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3637] [UniProtKB: O02824]
ChEMBL Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay F 8.4 pKd 3.98 nM Kd J Med Chem (1997) 40: 2674-2687 [PMID:9276013]
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
GtoPdb - - 9 pKi - - - J Biol Chem (2001) 276: 25366-71 [PMID:11331292]
ChEMBL Overall binding displacement in tissues containing only the Alpha-1A adrenergic receptor from rat submaxillary gland B 9.15 pKi 0.7 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL Binding affinity against Alpha-1B adrenergic receptor from hamster clones. B 6.27 pKi 535 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL The compound was tested for binding affinity against Alpha-1B adrenergic receptor, from human clones. B 7.04 pKi 92 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Binding affinity was tested on human Alpha-1B adrenergic receptor B 7.4 pKi 39.81 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
GtoPdb - - 7.7 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from human clones. B 7.68 pKi 21 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
GtoPdb - - 8 pKi - - - Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248];
Mol Pharmacol (1995) 48: 250-8 [PMID:7651358];
Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121];
Pharmacol Res Perspect (2020) 8: e00602 [PMID:32608144]
ChEMBL Binding affinity was tested on human Alpha-1D adrenergic receptor B 8 pKi 10 nM Ki J Med Chem (1997) 40: 1293-1315 [PMID:9135028]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Binding affinity against Alpha-1D adrenergic receptor, from rat clones. B 6.73 pKi 186 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
ChEMBL Overall binding displacement in tissues containing only the Alpha-1B adrenergic receptor (rat spleen, rat liver) B 7.02 pKi 96 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones. B 6.21 pKi 612 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Binding affinity against Alpha-2B adrenergic receptor from human clones. B 6.39 pKi 406 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Binding affinity against Alpha-2C adrenergic receptor from human clones. B 6.88 pKi 131 nM Ki J Med Chem (1995) 38: 3415-3444 [PMID:7658428]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]